Afoxolaner
(Synonyms: 阿福拉纳) 目录号 : GC39248
An isoxazoline insecticide and acaricide
Cas No.:1093861-60-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Afoxolaner is an isoxazoline insecticide and acaricide.1 It is a GABA receptor antagonist that inhibits GABA-induced currents in P. americana thoracic neurons (IC50 = 10.8 nM). It induces mortality in 100% of C. felis after 24 and 48 hours when used at concentrations of 0.32 and 0.16 ?g/ml in an artificial membrane blood feeding device. Afoxolaner (2.5 mg/kg) eradicates C. felis infestation in dogs for up to 42 days and D. variabilis infestation for up to 30 days. Formulations containing afoxolaner have been used in the prevention of flea and tick infestations in dogs.
1.Shoop, W.L., Hartline, E.J., Gould, B.R., et al.Discovery and mode of action of afoxolaner, a new isoxazoline parasiticide for dogsVet. Parasitol.201(3-4)179-189(2014)
| Cas No. | 1093861-60-9 | SDF | |
| 别名 | 阿福拉纳 | ||
| Canonical SMILES | O=C(C1=C2C=CC=CC2=C(C3=NOC(C(F)(F)F)(C4=CC(C(F)(F)F)=CC(Cl)=C4)C3)C=C1)NCC(NCC(F)(F)F)=O | ||
| 分子式 | C26H17ClF9N3O3 | 分子量 | 625.87 |
| 溶解度 | DMSO: ≥ 250 mg/mL (399.44 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5978 mL | 7.9889 mL | 15.9778 mL |
| 5 mM | 0.3196 mL | 1.5978 mL | 3.1956 mL |
| 10 mM | 0.1598 mL | 0.7989 mL | 1.5978 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Safety of oral Afoxolaner formulated with or without milbemycin oxime in homozygous MDR1-deficient collie dogs
J Vet Pharmacol Ther 2022 Jul;45(4):373-379.PMID:35536118DOI:10.1111/jvp.13064.
Afoxolaner, an insecticide and acaricide compound of the isoxazoline class, is available for dogs as an oral ectoparasiticide medicine (NexGard®) and as an oral endectoparasiticide medicine in combination with milbemycin oxime (MO), a macrocyclic lactone (NexGard® Spectra). The safety of these two compounds, alone or in combination, was investigated in homozygous MDR1-deficient collie dogs, in two studies. Overall, 30 adult collie dogs were treated once orally, 9 with a placebo, 9 with Afoxolaner, 6 with MO, and 6 with a combination of Afoxolaner and MO. For Afoxolaner, the mean investigated dosage corresponded to 3.8 and 4.7 multiples of the maximum recommended therapeutic doses (RTD) in NexGard® and NexGard® Spectra, respectively. For MO, the mean investigated dosage corresponded to 4.7 multiples of the maximum RTD in NexGard® Spectra. Dogs were closely monitored for adverse reactions on the day of treatment and for the following two days. No significant adverse reaction was observed in any dog from the Afoxolaner or the Afoxolaner + MO groups; in the MO-only treated group, mild and transient neurological signs were observed during the 4-8 h post-treatment window. These studies demonstrated a high level of safety of oral Afoxolaner, alone or in combination with milbemycin oxime, in homozygous MDR1-deficient dogs.
Efficacy of Afoxolaner for the treatment of ear mite infestation under field conditions
Vet Parasitol 2021 Dec;300:109607.PMID:34735846DOI:10.1016/j.vetpar.2021.109607.
Otodectes cynotis is a commonly occurring surface mite that can be easily transmitted between suitable hosts, including dogs, causing otocariosis. The activity of the systemic insecticide Afoxolaner against O. cynotis has been tested once under experimental conditions, showing a high efficacy. The present study aimed to i) assess the efficacy of two consecutive monthly oral administrations of Afoxolaner (NexGard®) against O. cynotis in naturally infested dogs under field conditions and ii) evaluate its impact in reducing bacteria or fungal secondary infections. Dogs, positive for O. cynotis (n = 20), were included in the study and allocated in two groups of ten animals each (G1, control group, and G2, treated group). The first group of ear mite-infested dogs was treated with a placebo, while Afoxolaner was administered orally to the second group of dogs at Day 0 (D0) and Day 30 (D30), following label instructions. Otoscopic assessments, deep-swab method and swab samples were performed on all dogs (Days 0, 30, 42) to evaluate the presence or absence of live mites and their number throughout the study, as well as to conduct bacterial and fungal assessments. No adverse events likely related were recorded throughout the study. By Day 42 (D42), all dog's ears were flushed to recover ear mites. All treated dogs became negative, as well as two dogs of the control group. The treatment efficacy of Afoxolaner was 100 % based on the arithmetic means of the live mite counts. The clinical scores did not change significantly in the control group, whereas they significantly improved in the treated one from D0 to D30 (p-value = 5.47 10-5). No live mites were present in the afoxolaner-treated group at D42 (p-value = 0.00073). In this field study, two oral administrations of Afoxolaner at the recommended dose allowed a complete cure of the infestation. Bacterial and Malassezia pachydermatis infections were detected in both groups, although no significant trend was associated to the ear mite treatment.
Insecticidal efficacy of Afoxolaner against Stomoxys calcitrans (Diptera: Muscidae) in dogs
Curr Res Parasitol Vector Borne Dis 2021 Jul 21;1:100043.PMID:35284852DOI:10.1016/j.crpvbd.2021.100043.
The insecticidal activity of oral Afoxolaner (NexGard®) against stable flies Stomoxys calcitrans (Diptera: Muscidae) that had fed on dogs was evaluated in a blinded, randomised, and negative controlled efficacy study. The efficacy assessments were based on survival rates of fed flies after challenges to treated dogs. For a challenge, each dog was exposed to 50 unfed S. calcitrans for 30 minutes, after which time live fed flies were collected and incubated in an insectarium for viability assessment after 48, 72 and 96 hours. Fourteen dogs were randomly allocated to an untreated control group and an afoxolaner-treated group of seven dogs each. NexGard® was administered on Day 0 per label instructions to the treated group. All dogs were challenged on Days 1, 7, 14, 21 and 28. Efficacy was calculated by comparison of the proportion of incubated live fed flies for each individual after their related 30-min challenges in the control and treated groups after 48, 72 and 96 hours of incubation. A significant Afoxolaner activity against S. calcitrans was demonstrated, with efficacy at 96 hours after blood-feeding ranging from 76.4 to 98.5% through Day 28.
Assessment of Afoxolaner efficacy against Otodectes cynotis infestations of dogs
Parasit Vectors 2016 Dec 9;9(1):635.PMID:27938395DOI:10.1186/s13071-016-1924-4.
Background: The efficacy of a single 2.5 mg/kg dose of Afoxolaner (NexGard®, Merial) against induced Otodectes cynotis infestations was assessed in eight afoxolaner-treated dogs, compared to eight untreated dogs. Methods: After O. cynotis infestations were established and confirmed by otoscopic assessments in 16 dogs, all of the dogs were included in the study and allocated to two separate treatment groups. The first group of eight ear mite-infested dogs remained untreated, while Afoxolaner was administered orally to the second group of dogs at the minimum recommended dose once on Day 0. Otoscopic assessments performed on all dogs (Days -7, -2, 14 and 28) confirmed the presence or absence of live mites throughout the study. No serious adverse events were recorded throughout the study, and no adverse events were likely related to the administration of NexGard. Results: By Day 28, seven out of eight untreated dogs were still infested with ear mites, while only two out of eight afoxolaner-treated dogs were infested, with one and four ear mites, respectively. On Day 28, the reductions of mite counts in the afoxolaner-treated group versus those of the control dogs were 98.5% based on geometric means, and 99.4% based on arithmetic means. Significantly fewer (P < 0.05) live mites were present in the afoxolaner-treated group than the untreated group on Day 28. Conclusion: The results of this study demonstrated that a single oral administration of Afoxolaner at the minimum recommended dose is highly effective (>98%) in treating dogs with induced O. cynotis infestations.
Insecticidal efficacy of Afoxolaner against bedbugs, Cimex lectularius, when administered orally to dogs
Parasite 2021;28:7.PMID:33528356DOI:10.1051/parasite/2021004.
The objective of this experimental study was to assess the insecticidal efficacy of Afoxolaner (NexGard®) against bedbugs (Cimex lectularius) on dogs. For each challenge, 20 bedbugs were placed in two chambers positioned in contact to the dog's skin for 15 min, after which live fed parasites were counted and incubated for survival evaluations. On Day 0, 7 dogs assigned to the treated group were administered Afoxolaner orally at the registered dose. All 14 dogs were challenged on Days 1, 7, 14, 21 and 28, and the collected live fed C. lectularius incubated for 72 h (Day 1), and 72 h and 96 h (Days 7, 14, 21 and 28) for survival evaluation. The percent feeding in the control group ranged from 95% to 98.6% and the percent of live fed bedbugs at 96 h ranged from 99.3% to 100% in the control group, demonstrating the viability of the strain and their capacity to feed on dogs. Significantly fewer live fed bedbugs were counted in the treated group, compared to the control group, at all time-points. The reduction of live fed C. lectularius in the Afoxolaner group was 41.4% at 72 h after the Day 1 challenge, and 77.2%, 82.7%, 85.0% and 63.5% at 96 h after the Days 7, 14, 21 and 28 challenges, respectively. It is hypothesized that monthly treatment of dogs with Afoxolaner could help in preventing a bed bug population from installing in a household if bedbugs bite dogs in the presence of humans.